AR030913A1 - A COMPOUND DERIVED FROM INDOLINA, ITS USE, A PROCEDURE TO PREPARE IT, A PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND A PROCEDURE TO PREPARE SUCH COMPOSITION - Google Patents

A COMPOUND DERIVED FROM INDOLINA, ITS USE, A PROCEDURE TO PREPARE IT, A PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND A PROCEDURE TO PREPARE SUCH COMPOSITION

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Publication number
AR030913A1
AR030913A1 ARP000104121A ARP000104121A AR030913A1 AR 030913 A1 AR030913 A1 AR 030913A1 AR P000104121 A ARP000104121 A AR P000104121A AR P000104121 A ARP000104121 A AR P000104121A AR 030913 A1 AR030913 A1 AR 030913A1
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AR
Argentina
Prior art keywords
alkyl
prepare
procedure
hydrogen
ring
Prior art date
Application number
ARP000104121A
Other languages
Spanish (es)
Inventor
Jonathan Richard Anthon Roffey
James Edward Paul Davidson
Howard Langham Mansell
Richard John Hamlyn
David Reginald Adams
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Vernalis Res Ltd
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Publication date
Application filed by Vernalis Res Ltd filed Critical Vernalis Res Ltd
Publication of AR030913A1 publication Critical patent/AR030913A1/en

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

Compuestos derivados de indolina de formula (1) en el que : R1 y R2 se seleccionan independientemente de hidrogeno y alquilo, R3 es alquilo, R4 y R5 se seleccionan de hidrogeno y alquilo, R6 y R7 se seleccionan independientemente de hidrogeno, halogeno, hidroxi, alquilo, arilo, amino, alquilamino, dialquilamino, alcoxi, ariloxi, alquiltio, alquilsulfoxilo, alquilsulfonilo, nitro, carbonitrilo, carboalcoxi, carboariloxi, y carboxilo, y A es un anillo de 5 a 6 eslabones que contiene opcionalmente uno o más heteroátomos, estando saturados o insaturados los átomos del anillo A distintos de los átomos de carbono insaturados del anillo de fenilo al que está condensado el anillo A; y las sales, compuesto de adicion y promedicamentos farmacéuticamente aceptables de estos; y el uso de estos en terapia, particularmente como agonistas o antagonistas de un receptor de 5-HT, particularmente en receptor de 5-HT2c, por ejemplo en el tratamiento de trastornos del sistema nervioso central, dano al sistema nervioso central, trastornos cardiovasculares, trastornos gastrointestinales, diabetes insípida y apnea del sueno y particularmente para el tratamiento de la obesidad.Indoline-derived compounds of formula (1) in which: R1 and R2 are independently selected from hydrogen and alkyl, R3 is alkyl, R4 and R5 are selected from hydrogen and alkyl, R6 and R7 are independently selected from hydrogen, halogen, hydroxy , alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carboalkoxy, carboaryloxy, and carboxyl, and A is a 5 to 6 link ring optionally containing one or more heteroatoms, the atoms of ring A other than the unsaturated carbon atoms of the phenyl ring to which ring A is condensed are saturated or unsaturated; and salts, compound of pharmaceutically acceptable addition and averages thereof; and the use of these in therapy, particularly as agonists or antagonists of a 5-HT receptor, particularly in 5-HT2c receptor, for example in the treatment of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus and sleep apnea and particularly for the treatment of obesity.

ARP000104121A 1999-08-11 2000-08-10 A COMPOUND DERIVED FROM INDOLINA, ITS USE, A PROCEDURE TO PREPARE IT, A PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND A PROCEDURE TO PREPARE SUCH COMPOSITION AR030913A1 (en)

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GBGB9918965.6A GB9918965D0 (en) 1999-08-11 1999-08-11 Chemical compounds xxi

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AR030913A1 true AR030913A1 (en) 2003-09-03

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US (10) US6962939B1 (en)
EP (1) EP1202964B1 (en)
JP (1) JP2003507366A (en)
KR (2) KR20020015077A (en)
CN (1) CN1167681C (en)
AR (1) AR030913A1 (en)
AT (1) ATE306470T1 (en)
AU (1) AU774337B2 (en)
BR (1) BR0013314A (en)
CA (1) CA2377637A1 (en)
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PE (1) PE20010575A1 (en)
TR (1) TR200200351T2 (en)
UY (1) UY26290A1 (en)
WO (1) WO2001012602A1 (en)
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GB9918965D0 (en) * 1999-08-11 1999-10-13 Cerebrus Ltd Chemical compounds xxi
SE0004245D0 (en) 2000-11-20 2000-11-20 Pharmacia Ab Novel compounds and their use
AU1529402A (en) 2000-11-20 2002-05-27 Biovitrum Ab Piperazinylpyrazines compounds as antagonists of serotonin 5-ht2 receptor
WO2002074746A1 (en) * 2001-03-16 2002-09-26 Yamanouchi Pharmaceutical Co., Ltd. Benzazepine derivatives
BR0211140A (en) * 2001-07-13 2005-10-25 Upjohn Co Compounds and compositions of hexahydroazepine (4,5-g) indoles and indolines as 5-ht receptor binders
TWI312781B (en) 2002-04-25 2009-08-01 [1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
TW200307540A (en) * 2002-04-25 2003-12-16 Wyeth Corp [1, 4]Diazocino[7, 8, 1-hi] indole derivatives as antipsychotic and antiobesity agents
TW200307682A (en) 2002-04-25 2003-12-16 Wyeth Corp 1,2,3,4,7,8-Hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents
DE60330864D1 (en) 2002-06-19 2010-02-25 Biovitrum Ab Publ NEW CONNECTIONS, THEIR USE AND MANUFACTURE
CL2004000826A1 (en) 2003-04-25 2005-03-04 Pfizer USE OF AN AGONIST FOR THE 5-HT2C RECEPTOR TO PREPARE A USEFUL MEDICINAL PRODUCT IN THE TREATMENT OF URINARY INCONTINENCE CAUSED BY STRESS, WITH THE CONDITION THAT THE AGONIST IS NOT 1- [6-CHLORINE-5- (TRIFLUOROMETIL) -2- PIRIDINIL] PIPERAZINA (ORG-129
GB0314967D0 (en) 2003-06-26 2003-07-30 Hoffmann La Roche Piperazine derivatives
AR046890A1 (en) * 2003-12-15 2005-12-28 Alcon Inc [1,4] OXAZINO [2,3-G] SUBSTITUTED INDAZOLS FOR THE TREATMENT OF GLAUCOMA.
WO2006022420A1 (en) 2004-08-25 2006-03-02 Takeda Pharmaceutical Company Limited Preventives/remedies for stress urinary incontinence and method of screening the same
GT200500317A (en) 2004-11-05 2006-10-27 PROCESS TO PREPARE QUINOLINE COMPOUNDS AND PRODUCTS OBTAINED FROM THEM
US7425572B2 (en) 2004-12-08 2008-09-16 Alcon, Inc. Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma
AR054849A1 (en) 2005-07-26 2007-07-18 Wyeth Corp DIAZEPINOQUINOLINAS, SYNTHESIS OF THE SAME, AND INTERMEDIARIES TO OBTAIN THEM
US20090203750A1 (en) * 2005-08-24 2009-08-13 Alan Kozikowski 5-HT2C Receptor Agonists as Anorectic Agents
EP2727585A1 (en) 2006-05-16 2014-05-07 Takeda Pharmaceutical Company Limited In-vivo screening method
DE102006033114A1 (en) * 2006-07-18 2008-01-24 Grünenthal GmbH Spirocyclic azaindole derivatives
EP2789338A3 (en) 2007-11-15 2015-01-14 Takeda Pharmaceutical Company Limited Condensed pyridine derivate and use thereof
WO2011071136A1 (en) 2009-12-11 2011-06-16 アステラス製薬株式会社 Therapeutic agent for fibromyalgia
WO2011097336A2 (en) 2010-02-04 2011-08-11 The Board Of Trustees Of The University Of Illinois Highly selective 5-ht(2c) receptor agonists having antagonist activity at the 5-ht(2b) receptor
ES2889876T3 (en) 2015-01-29 2022-01-14 Univ Illinois Cyclopropylmethanamines as selective 5-HT(2C) receptor agonists
WO2018151239A1 (en) * 2017-02-17 2018-08-23 第一三共株式会社 3, 6-DIHYDRO-2H-FURO[2, 3-e]INDOLE COMPOUND
WO2018151240A1 (en) * 2017-02-17 2018-08-23 第一三共株式会社 3,6,7,8-TETRAHYDROCYCLOPENTA[e]INDOLE COMPOUND
EP3733204A4 (en) 2017-12-27 2021-09-15 Takeda Pharmaceutical Company Limited Therapeutic agent for stress urinary incontinence and fecal incontinence

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2541211A (en) 1948-10-15 1951-02-13 Searle & Co Tertiary-aminoalkyl-tetrahydrocarbazoles
US2687414A (en) 1948-11-26 1954-08-24 Searle & Co Method for producing aromatic aminoalkyl amines
DE930988C (en) 1953-01-01 1955-07-28 Bayer Ag Process for the preparation of basic alkylated tetrahydrocarbazoles or indoles
US3329571A (en) 1961-10-24 1967-07-04 American Home Prod Methods for treating depression
US3142678A (en) 1962-01-09 1964-07-28 American Home Prod Amino substituted penthienoindoles
TW270114B (en) 1993-10-22 1996-02-11 Hoffmann La Roche
TW334423B (en) 1993-10-22 1998-06-21 Hoffmann La Roche Tricyclic 1-aminoethylpyrrole-derivatives
GB9326192D0 (en) * 1993-12-22 1994-02-23 Glaxo Group Ltd Chemical compounds
TW403738B (en) 1994-08-12 2000-09-01 Hoffmann La Roche Tricyclic pyrazole derivatives
FR2742047B1 (en) * 1995-12-06 1998-01-16 Oreal KERATINIC FIBER DYEING COMPOSITIONS CONTAINING N-SUBSTITUTED DERIVATIVES OF 4-HYDROXY INDOLINE, NEW DERIVATIVES, THEIR SYNTHESIS METHOD, THEIR USE FOR DYEING, AND THE DYEING METHOD
AU5343298A (en) 1997-01-13 1998-08-03 Yamanouchi Pharmaceutical Co., Ltd. 5-ht2c receptor agonists and aminoalkylindazole derivatives
AU727654B2 (en) * 1997-06-13 2000-12-21 Yamanouchi Pharmaceutical Co., Ltd. Tricyclic pyrazole derivative
GB9819019D0 (en) 1998-09-01 1998-10-28 Cerebrus Ltd Chemical compounds II
GB9819033D0 (en) * 1998-09-01 1998-10-28 Cerebrus Ltd Chemical compounds VI
GB9819035D0 (en) 1998-09-01 1998-10-28 Cerebrus Res Ltd Chemical compounds VII
GB9918962D0 (en) 1999-08-11 1999-10-13 Cerebrus Ltd Chemical compounds xxii
GB9918965D0 (en) * 1999-08-11 1999-10-13 Cerebrus Ltd Chemical compounds xxi

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